RGNCY-0009 (CDK2-4 Inhibitor)
Cancer is characterized by the uncontrolled proliferation of cells. The
biochemical processes which control a cell’s progression though the cell
cycle are critical to this process. The cyclin dependent kinases CDK4
and CDK6 are key regulators of the transition though G1 phase.
RGNCY-0009 is a potent inhibitor of CDK 2 (IC50 = 0.159uM) and CDK4
(IC50 = 0.0038uM) in addition to activity against ARK5, FGFR1, PDGFRb,
and PI3K-d. RGNCY-0009 has demonstrated a GI50 of 0.025 uM for both
Granta-519 and mantle cell lymphoma cell lines.
Systematic Name: 8-cyclopentyl-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carbonitrile
SMILES: CN1CCN(C2=CC=C(NC3=NC=C4C(N(C5CCCC5)C(C(C#N)=C4)=O)=N3)C=C2)CC1
Molecular Weight: 429.52
Formula: C24H27N7O
PMID: 24417566
Reference: Reddy, MV Ramana, et al. "Discovery of 8-Cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7, 8-dihydro-pyrido [2, 3-d] pyrimidine-6-carbonitrile (7x) as a Potent Inhibitor of Cyclin-Dependent Kinase 4 (CDK4) and AMPK-Related Kinase 5 (ARK5)." Journal of Medicinal Chemistry 57.3 (2014): 578-599.
Tags: CDK4, CDK2, Cancer, lymphoma, RGNCY-0009, ARK5, FGFR1, PDGFRb, PI3K-d
